芋螺毒素研究进展

芋螺毒素是含约１０－３０个氨基酸残基的小肽，大多富含二硫键，可分为α－，μ，ω－，δ－，芋螺睡眠肽，加压素，惊厥剂等。已确定四十余个毒素的序列，对４个有代表性的芋螺肽进行了溶液构象分析和构效关系的研究。本文介绍了芋螺毒素研究历史。综述了国外对甚至芋螺毒素的构效关系研究的结果及应用研究情况。

PROGRESS IN THE INVESTIGATION ON CONOTOXINS

This review largely deals with the peptide toxins elaborated by marine cone snails of the genus Conus . Each species of Conus contains in its venom 50 to 200 different peptides directed at different macromolecular targts. These include competitive antagonists of postsynaptic nicotinic receptors (a-conotoxins), blockers selective for Na+ channels in skeletal muscle (u- conotoxins), blockers of presynaptic of antagonists of postsynaptic Ca2+ channels (w-conotoxins), activators of Na+ channels (s-conotoxins), blockers of K+ channels (k-conotoxins), blockers of nicotinic receptor channels (u-conotoxins) and antagonists of NMDA receptors (cono-sleeper). The small size of the peptides (13 to 30 residues is typical) has facilitated synthesis of many of them. A very attractive feature is the highly cross-linked conserved 2 to 3 disulfide bonds which make conotoxins conformationally rigid, some of conotoxins, however, are stabilized by r-carboxyglutamates. The Structure-Activity Relationships of conotoxins and a brief perspective have been reviewed in the paper.